In the past several decades, both the incidence and the types of fungus infection severely detrimental to human health were continuously increased, especially for the immunosuppressed patients. During this period, the clinical application of certain commonly used antifungal agents, such as amphotericin, imidazoles and triazoles, was restricted due to significant neurotoxicity, drug resistance, and the like. Echinocandins, as a kind of novel antifungal agents, are a group of natural products discovered in the 1970s. Structurally, the echinocandins have a similar cyclic polypeptide core but have different fatty acid side chains. Echinocandins can competitively inhibit the synthesis of β-D-glucan in fungal cell walls. The advantages of echinocandins are low toxicity, strong fungicidal activity, and as well as excellent pharmacokinetic properties.
Echinocandins family includes the following members: WF11899A, echinocandins, cilofungin, pneumocandins, aculeacins, and mulundocandin, with Micafungin, echinocandins and pneumocandins being actively investigated and currently applied clinically.
Micafungin is a water-soluble lipopeptide antifungal agent of echinocandins, which is obtained by chemically modifying the fermentation product from Coleophoma empetri. Micafungin has been developed by Fujisawa as a broad-spectrum antifungal agent. In an open study for patients with deep fungal infection (Candida or Aspergillus) conducted in Japan, 92% of the average efficiency can be reached after treating for about 22 days for each dose group. In a monocentre study conducted in the U.S. for 14 cases of cancer patients with candidemia, 50˜150 mg of Micafungin is used in combination with other anti-fungus agents or without any other anti-fungus agent, and it was found that 11 cases were effective among 12 cases (92%). These kinds of drugs are superior to traditional antifungal agents, due to non-hemolytic toxicity and less drug interaction.

Coleophoma empetri can produce a class of natural anti-fungus agents, such as the compounds of Formula I, II, III.
The productivity of Coleophoma empetri (Accession No. FERM BP-2635) for the compound of Formula I is very low (merely 700 mg/L), therefore, the cost for industrialization will be very high.
General Formula I, II, III

Formula I R1═OH, R2═OH
Formula II R1═OH, R2═H
Formula III R1═H, R2═H
Accordingly, it is urgent to find a strain with stable genetic and high-yield properties which can produce more of the compound of Formula I for fulfilling the requirements of industrial production.